ライフサイエンスコーパス: CYP2A6

1 ed to be proxies for functional variation in CYP2A6.

2 stallography and compared with structures of CYP2A6.

3 ulations due to differences in metabolism by CYP2A6.

4 es NNK with much lower K(m) values than does CYP2A6.

5 activity relationship (SAR) of inhibition of CYP2A6.

6 nicotine complexes with CYP2A13 (2.5 A) and CYP2A6 (2.3 A) yield a structural rationale for the pref

7 ), 9 [DBH] (p-value = 9.69 x 10(-9)) and 19 [CYP2A6/7] (p-value = 3.49 x 10(-8)) and for FEV1/FVC on

8 was characterized and compared with that of CYP2A6, a human ortholog of rat CYP2A3, which has been d

9 e to genetic polymorphisms in CYP2B6, NR1I3, CYP2A6, ABCB1, ABCB5, and ABCG2.

10 Evidence is presented that CYP2A6 accommodates multiple ligands and that intramolec

11 ine at inhibition of coumarin 7-hydroxylase (CYP2A6) activity.

12 disease susceptibility (HHIP, IREB2/CHRNA3, CYP2A6/ADCK, TGFB2, and MMP12).

13 the predictive model by including additional CYP2A6 alleles improves the fit of the model in an indep

14 simplify the range of function of different CYP2A6 alleles, their numerous possible diplotype combin

15 Amino acid differences between CYP2A6 and CYP2A13 at positions 117, 300, 301, and 208 r

16 redox transitions of the haem domain in both CYP2A6 and CYP2A6-FLD.

17 the product were performed with immobilized CYP2A6 and CYP2A6-FLD.

18 enes encoding nicotine-metabolizing enzymes (CYP2A6 and CYP2B6) and nicotinic acetylcholine receptor

19 is of a previous study, we hypothesized that CYP2A6 and CYP2E1 accommodate multiple xylene ligands.

20 at P450 enzymes bound to either b5 alpha4-5 (CYP2A6 and CYP2E1) or this region and alpha2-3 (CYP2D6 a

21 on of cytotoxicity and inhibition of hepatic CYP2A6 and CYP3A4 showed that 44 fulfills first safety c

22 Here, we demonstrate that when CYP2A6 and EGLN2 genotypes are analyzed together, the ke

23 Although both the hepatic CYP2A6 and respiratory CYP2A13 enzymes metabolize these

24 rst reported electrochemical signal of human CYP2A6 and to improve its catalytic efficiency on electr

25 This region includes RAB4B, EGLN2, MIA and CYP2A6, and has previously been identified in associatio

26 elective enzymatic CYP inhibitors identified CYP2A6 as the major isoform involved in this process.

27 ated with nicotine metabolism independent of CYP2A6, but is nevertheless independently associated wit

28 that compliment the active site features of CYP2A6 can exhibit significant selectivity for CYP2A6 re

29 The CYP2A3 and CYP2A6 cDNAs were cloned into baculovirus, and recombina

30 X-ray crystal structures of CYP2A6 cocrystallized with three furan analogues bearing

31 human CYP2A subfamily comprises three genes, CYP2A6, CYP2A7, and CYP2A13.

32 this methylation-based screen--the vanin and CYP2A6-CYP2A7 gene clusters--both implicated in traits o

33 Apo-b(5) enhances the activities of CYP3A4, CYP2A6, CYP2C19, and CYP17A1 but not that of CYP2E1 or C

34 A predictive model that translates CYP2A6 diplotype into a single continuous variable was p

35 Because the CYP2A6 effect was seen only in smokers, these data sugge

36 CYP2A6 exhibited cooperative kinetics for m-xylene-alpha

37 DRD2 exhibits significant homophily and that CYP2A6 exhibits significant heterophily.

38 ta: rs113288603 is associated with increased CYP2A6 expression in cerebellar hemispheres (p = 7.8 x 1

39 electrochemical activity of the immobilized CYP2A6-FLD, toward both coumarin and nicotine substrates

40 with a higher efficiency by the immobilized CYP2A6-FLD, with a calculated kcat value significantly h

41 vibrio vulgaris (FLD) to create the chimeric CYP2A6-FLD.

42 itions of the haem domain in both CYP2A6 and CYP2A6-FLD.

43 t were performed with immobilized CYP2A6 and CYP2A6-FLD.

44 Variation in the CYP2A6 gene alters the rate of nicotine metabolic inacti

45 es because of polymorphic differences in the CYP2A6 gene.

46 erved in rat CYP2A3, mouse Cyp2a5, and human CYP2A6 genes and was found to be essential for transcrip

47 CYP2A6 genotype is not associated with nicotine dependen

48 A significant CYP2A6 genotype x smoking effect was found in the dorsal

49 he relationship between Cytochrome P450 2A6 (CYP2A6) genotype and smoking phenotypes made comparisons

50 Thus, rat CYP2A3 and human CYP2A6 have differences in substrate specificity as well

51 hylphenylamine but was much less active than CYP2A6 in coumarin 7-hydroxylation.

52 , the expressed CYP2A13 was more active than CYP2A6 in the metabolic activation of hexamethylphosphor

53 , by tranylcypromine, a potent and selective CYP2A6 inhibitor.

54 The inhibitory activity of the most potent CYP2A6 inhibitors on the functional activity of human cy

55 he conclusion that the finding is related to CYP2A6 involvement in nicotine metabolism.

56 CYP2A6 is active toward many carcinogens and is the majo

57 Another cytochrome P450, CYP2A6, is also present in human lung, but at much lower

58 nhibited coumarin 7-hydroxylation by RLM and CYP2A6 (Ki, 3000 and 320 microM, respectively).

59 ation and supported findings that CYP2D6 and CYP2A6 mediated this reaction.

60 ted with structural changes in the brain and CYP2A6 mediates these changes.

61 AHR), 15q24 (near CYP1A2) and 19q13.2 (near CYP2A6) met GW-significance (P < 5 x 10-8) and were asso

62 sly reported in a region of 19q13, including CYP2A6 (nicotine metabolism enzyme) and EGLN2 (hypoxia r

63 s, and ( k H/ k D) obs values for CYP2E1 and CYP2A6 oxidation of m-xylene-alpha- (2)H 3 and p-xylene-

64 asure of hepatic nicotine metabolism via the CYP2A6 pathway and total nicotine clearance, is a predic

65 or deciphering the metabolic implications of CYP2A6 polymorphism and for the screening of CYP2A6 subs

66 favirenz exposure were defined by CYP2B6 and CYP2A6 polymorphisms.

67 , and several exhibited high selectivity for CYP2A6 relative to CYP2E1, -3A4, -2B6, -2C9, -2C19, and

68 P2A6 can exhibit significant selectivity for CYP2A6 relative to other human liver drug-metabolizing P

69 identified a significant association between CYP2A6 rs113288603 and hearing loss symptoms (p = 5.75 x

70 As expected, the overall CYP2A13 and CYP2A6 structures are very similar with an average root

71 CYP2A6 polymorphism and for the screening of CYP2A6 substrates and inhibitors.

72 Like CYP2A6, the CYP2A13 active site cavity is small and high

73 This work shows that CYP2A6 turnover efficiency is improved when the protein

74 highly selective for the inhibition of human CYP2A6 versus the other human CYPs examined.

75 Km for rat CYP2E1, human CYP2E1, and human CYP2A6 was 210, 115, and 17 microM, respectively (Vmax:

76 On the other hand, CYP2A6 was active toward coumarin but not toward testost

77 the selectivity of the phenyl analogues for CYP2A6 was decreased relative to the pyridyl compounds.

78 In contrast, the activity of CYP2A6 was only weakly inhibited by metyrapone or methox

79 tochrome P450 Family 2 Subfamily A Member 6 (CYP2A6), we investigated the human phenome in a total of

80 ll microsomal fractions containing CYP2A3 or CYP2A6 were studied in a reconstituted system with purif

81 ignificantly higher (P < 0.005) than that of CYP2A6, whereas the affinity for the substrate (KM) rema